Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : MI-3454
CAS No.: 2134169-43-8
Catalog No.: PC-72046Not For Human Use, Lab Use Only.
MI-3454 (MI 3454) is a highly potent, orally bioavailable inhibitor of the menin-MLL1 interaction with IC50 of 0.51 nM, 60-fold improvement over MI-503.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 1 mg | $198 | In stock | |
| 5 mg | $458 | In stock | |
| 10 mg | $758 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
MI-3454 (MI 3454) is a highly potent, orally bioavailable inhibitor of the menin-MLL1 interaction with IC50 of 0.51 nM, 60-fold improvement over MI-503.
MI-3454 inhibits growth of human MLL leukemic cell lines (MLL-tr): MV-4-11, MOLM-13, KOPN-8, SEM, RS4-11 with GI50 values of 7-27 nM in MTT cell viability assays, does not significantly (>100-fold) affect the growth of leukemic cells without MLL1 translocations.
MI-3454 (50 nM or lower) led to downregulated expression of HOXA9 and MEIS1 in MV-4-11 and MOLM13 cells, also reduced other MLL fusion target genes, including MEF2C, DLX2, HOXA10, PBX3, and FLT3.
MI-3454 demonstrated strong reduction of cell proliferation and downregulation of HOXA9 and MEIS1 expression in mouse bone marrow cells transformed with the MLL-AF9 oncogene but not in bone marrow cells transformed with HOXA9 and MEIS1 oncogenes.
MI-3454 induces leukemia regression in xenograft model of MLL leukemia through on-target activity.
MI-3454 (3–12 nM) substantially reduced clonogenic potential in MLL leukemia patient samples with MLL1 translocations or NPM1 mutations, MI-3454 induced complete remission or blocks leukemia progression in PDX models of MLL leukemia.
| M.Wt | 636.742 | |
| Formula | C32H35F3N8OS | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
Formamide, N-[3-[[2-cyano-4-methyl-5-[[4-[[2-(methylamino)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-1H-indol-1-yl]methyl]bicyclo[1.1.1]pent-1-yl]- |
|
1. Klossowski S, et al. J Clin Invest. 2020 Feb 3;130(2):981-997.
2. Miao H, et al. Blood. 2020 Dec 17;136(25):2958-2963.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
